HDAC2-IN-1
HDAC2-IN-1 (Compound 17) is a brain penetrant, orally active, competitive HDAC2 inhibitor with an IC50 of 0.5 μM. HDAC2-IN-1 also inhibits HDAC1 and HDAC8 with IC50s of 1.61 μM and 0.98 μM, respectively.
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- CAS No.: 2919691-32-8
- Formule: C22H23ClN4OS
- Masse moléculaire:426.96
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Description
IC50 & Target
[1]|
HDAC2 0.5 μM (IC50) |
HDAC8 0.98 μM (IC50) |
HDAC1 1.61 μM (IC50) |
In Vitro
HDAC2-IN-1 (Compound 17) (3 and 10 μM; 48 h) increases histone H4K12 and H3K9 acetylation levels in SKNSH cells in a dose-dependent manner[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male C57BL/6 mice[1]
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Dosage:30 or 100 mg/kg
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Administration:Oral administration (Pharmacokinetic Analysis)
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Result:Showed good plasma and brain exposure, also showed promising brain penetration, Kp,uu = 0.36. Significantly increased histone H4K12 acetylation in mouse brain 4 h after oral dosing at 100 mg/kg.
Chemical Information
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CAS No. 2919691-32-8
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Masse moléculaire 426.96
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Formule C22H23ClN4OS
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SMILES
ClC1=CC([C@@H]2C[C@H](C(N3CCN(CC3)C4=NC=CC5=C4SC=C5)=O)NC2)=CC=C1
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocole
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
HDAC2-IN-1 Related Classifications
HY-151248 Related Classifications
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